(S)-PFI-2 (hydrochloride) - CAS:1627607-88-8

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(S)-PFI-2 (hydrochloride)

目录号 : KCM11825 CAS No. : 1627607-88-8 纯度 : ≥95%

Data Sheet 产品使用指南

SET domain-containing protein 7/9 (SET7/9) is a histone methyltransferase that monomethylates lysine 4 of histone H3, which generates a specific tag for epigenetic transcriptional activation. It plays a role in the transcriptional activation of tumor suppressor p53 in response to DNA damage, as well as the transcription factor TAF10. (R)-PFI-2 is a potent, cell-permeable inhibitor of SET7/9 (IC = 2 nM) that demonstrates greater than 1,000-fold selectivity over a panel of 18 other methyltransferases. (S)-PFI-2, the inactive enantiomer, is 500-fold less potent (IC = 1 µM) and may serve as a negative control. See the Structural Genomics Consortium (SGC) website for more information.

规格	价格	是否有货	数量
1mg		In-stock
5mg		In-stock
10mg		In-stock

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生物活性

(S)-PFI-2 (hydrochloride) is an inhibitor of lysine methyltransferase SETD7 and is approximately 500-fold more active than its enantiomer (R)-PFI-2. (R)-PFI-2 is a cofactor-dependent and substrate-competitive inhibitor. (R)-PFI-2 can occupy the substrate peptide binding groove of SETD7 (including the catalytic lysine binding channel) and interact with the cofactor The donor methyl group is in direct contact. However, (S)-PFI-2 was not observed to have the same interaction as (R)-PFI-2.

IC₅₀&Target

Lysine methyltransferase SETD7

体外研究

(S) PFI-2 (hydrochloride) (10 μM; 2 h) did not cause a dose-dependent increase in nuclear YAP in MCF7 cells, nor did it enhance the expression of YAP target genes AREG and CYR61; And (R) - PFI-2 can increase the expression of YAP, AREG, and CYR61 [1].

分子式

C₂₃H₂₅F₄N₃O₃S^.HCl

分子量

535.98

CAS号

1627607-88-8

中文名称

(S)-PFI-2 (hydrochloride)

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

纯度： ≥95%

Data Sheet

产品使用指南

[1]. Niu Y, et al. Revealing inhibition difference between PFI-2 enantiomers against SETD7 by molecular dynamics simulations, binding free energy calculations and unbinding pathway analysis. Sci Rep. 2017 Apr 18;7:46547.

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

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注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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动物实验计算换算器